Farajzadeh Öztürk Nazlı, Zengin Uzunmehmetoğlu Hilal, Yenilmez Hacer Yasemin, Özdemir Sadin, Dündar Abdurrahman, Altuntaş Bayır Zehra
Department of Analytical Chemistry, Faculty of Pharmacy, Acıbadem Mehmet Ali Aydınlar University, Ataşehir, TR-34752 Istanbul, Turkey.
Department of Chemistry, Istanbul Technical University, Maslak, TR-34469 Istanbul, Turkey.
ACS Omega. 2025 Jul 3;10(27):28709-28720. doi: 10.1021/acsomega.4c08762. eCollection 2025 Jul 15.
This study aims to design multidisciplinary bioagents for a wide range of biological applications. The synthesis and characterization of 4,5-bis-((4-phenylthiazol-2-yl)-thio)-phthalonitrile () and its octa-substituted zinc-(II) phthalocyanine derivative () were described in this study. Additionally, gold nanoparticles were synthesized in three different sizes, including 10 nm (), 45 nm (), and 80 nm (). Macromolecule () was used for surficial functionalization of gold nanoparticles () to prepare nanoconjugates (). Antioxidant, antimicrobial, antibacterial, antibiofilm, antidiabetic, and deoxyribonucleic acid (DNA) cleavage activities of biocandidates (, , and ) were examined to determine the optimum size of gold nanoparticles and the effect of modifying groups on their bioactivity in this study for the first time. The highest antioxidant activities were obtained for biocandidates ( and ) at 100 mg/L. The best minimum inhibitory concentration (MIC) values were obtained at 32 mg/L for bioagents (, , and ) against . whereas the MIC value was obtained at 32 mg/L for against . and . . Bioagents ( and ) exhibited high APDT activities (16 mg/L) against the studied microorganisms. The highest biofilm inhibition activities were obtained 94.57 and 89.28% for 50 mg/L nanoconjugate () against . and . , respectively. All the studied biocandidates inhibited 100% . viability at 50 mg/L. The antidiabetic activities of biocandidates (, , and ) were obtained between 7.52 and 100 mg/L. Bioagents (, , , and ) destroyed the DNA integrity, as well. The significant improvement in the biological activities of gold nanoparticles confirmed that new nanoconjugates especially can be considered promising medical nanomaterials after further clinical investigation.
本研究旨在设计用于广泛生物应用的多学科生物制剂。本研究描述了4,5-双-((4-苯基噻唑-2-基)-硫代)-邻苯二甲腈（）及其八取代锌-(II)酞菁衍生物（）的合成与表征。此外，还合成了三种不同尺寸的金纳米颗粒，包括10纳米（）、45纳米（）和80纳米（）。大分子（）用于金纳米颗粒（）的表面功能化，以制备纳米共轭物（）。本研究首次检测了生物候选物（、和）的抗氧化、抗微生物、抗菌、抗生物膜、抗糖尿病和脱氧核糖核酸（DNA）切割活性，以确定金纳米颗粒的最佳尺寸以及修饰基团对其生物活性的影响。生物候选物（和）在100毫克/升时获得最高抗氧化活性。生物制剂（、和）对的最佳最低抑菌浓度（MIC）值在32毫克/升时获得，而对和的MIC值在32毫克/升时获得。生物制剂（和）对所研究的微生物表现出高光动力疗法（APDT）活性（16毫克/升）。50毫克/升纳米共轭物（）对和的生物膜抑制活性分别达到94.57%和89.28%，为最高。所有研究的生物候选物在50毫克/升时均能100%抑制的活力。生物候选物（、和）的抗糖尿病活性在7.52至100毫克/升之间。生物制剂（、、和）也破坏了DNA完整性。金纳米颗粒生物活性的显著提高证实，经过进一步临床研究后，新的纳米共轭物尤其是有望成为有前景的医用纳米材料。
